Ibuclin^® Express (Powder) Instructions for Use

Marketing Authorization Holder

Dr. Reddy’s Laboratories Ltd. (India)

ATC Code

M01AE51 (Ibuprofen in combination with other drugs)

Active Substances

Ibuprofen (Rec.INN registered by WHO)

Paracetamol (Rec.INN registered by WHO)

Dosage Form

Ibuclin® Express

Powder for oral solution 400 mg+325 mg/1 sachet: sachet 5 g 6 or 9 pcs.

Dosage Form, Packaging, and Composition

Powder for oral solution from white to almost white in color, with a characteristic odor.

Excipients: sucrose, betadex (beta-cyclodextrin), sucralose, cherry flavor 501027 AP0551 [maltodextrin (corn), flavoring substances, benzyl alcohol (E1519), natural flavoring substances, triethyl citrate (E1505), flavoring preparations], orange flavor 4153 [maltodextrin (corn), natural flavoring preparations, acacia gum (E414), nature-identical flavors, dl-alpha-tocopherol (E307), butylated hydroxyanisole (E320), tert-butylhydroquinone (E319)], vanilla flavor SC295824 [maltodextrin (corn), acacia gum (E414), flavoring substances (vanillin, benzyl benzoate, piperonal, natural flavoring preparation (Peru balsam)].

5 g – sachets made of combined material (6) – cardboard packs.
5 g – sachets made of combined material (9) – cardboard packs.

Clinical-Pharmacological Group

Combination analgesic-antipyretic

Pharmacotherapeutic Group

Combined analgesic agent (NSAID + non-narcotic analgesic agent)

Pharmacological Action

A combined medicinal product containing ibuprofen (NSAID) and Paracetamol (analgesic-antipyretic).

Ibuprofen has analgesic, anti-inflammatory, and antipyretic effects. By inhibiting COX-1 and COX-2, it disrupts arachidonic acid metabolism, reduces the amount of prostaglandins (mediators of pain, inflammation, and hyperthermic response), both in the inflammation focus and in healthy tissues, and suppresses the exudative and proliferative phases of inflammation.

Paracetamol non-selectively blocks COX, predominantly in the CNS, has a weak effect on water-salt balance and the gastrointestinal mucosa. It has analgesic and antipyretic effects. In inflamed tissues, peroxidases neutralize the effect of paracetamol on COX-1 and COX-2, which explains the low anti-inflammatory effect.

Pharmacokinetics

Ibuprofen. Absorption is high. C_max in plasma is reached 1-2 hours after administration. Plasma protein binding is 90%. T_1/2 is 2 hours. It slowly penetrates into the joint cavity, is retained in the synovial tissue, creating higher concentrations there than in plasma. After absorption, about 60% of the pharmacologically inactive R-form slowly transforms into the active S-form. It undergoes metabolism. Excreted by the kidneys (unchanged not more than 1%) and, to a lesser extent, with bile.

Paracetamol. Absorption is high. C_max in plasma is reached 0.5-2 hours after administration. Plasma protein binding is 15%. Penetrates the BBB. Metabolized in the liver (90-95%): 80% undergoes conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form inactive metabolites. With glutathione deficiency, these metabolites can block hepatocyte enzyme systems and cause their necrosis. The isoenzyme CYP2E1 is also involved in the drug’s metabolism. T_1/2 is 1-4 hours. Excreted by the kidneys as metabolites, mainly conjugates. Less than 5% is excreted unchanged. T_1/2 is 4-5 hours.

Indications

For adults: moderate intensity pain syndrome; traumatic inflammation of soft tissues and the musculoskeletal system (including bruises, sprains, dislocations, fractures); postoperative period; primary dysmenorrhea; toothache; neuralgia; myalgia; lumbago; fibrositis; tenosynovitis; headache; febrile syndrome; joint syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gouty arthritis); sinusitis; tonsillitis.

For children (as an auxiliary medicinal product): tonsillitis; acute infectious and inflammatory diseases of the upper respiratory tract (pharyngitis, tracheitis, laryngitis).

ICD codes

Dosage Regimen

Administer orally. Dissolve the entire contents of one sachet in a glass of water immediately before use.

For adults and adolescents over 18 years of age, use one sachet every 6 to 8 hours as needed for pain or fever. Do not exceed three sachets in 24 hours.

The maximum duration of self-administered treatment without medical consultation is 3 days for fever and 5 days for pain. Discontinue use and consult a physician if symptoms persist or worsen.

For children and adolescents under 18 years of age, use only dosage forms specifically approved for the corresponding age category. This formulation is not intended for children under 18.

Leave at least 6 hours between doses. Use the lowest effective dose for the shortest duration necessary to relieve symptoms.

Avoid concomitant use with other products containing paracetamol or ibuprofen to prevent overdose.

In patients with mild to moderate hepatic impairment or mild renal impairment (creatinine clearance 30-60 ml/min), consider a reduced dose or increased dosing interval and use under close medical supervision. Contraindicated in severe hepatic or renal impairment.

For elderly patients, initiate treatment at the lower end of the dosing range. Monitor for adverse effects due to increased susceptibility.

Adverse Reactions

From the digestive system: NSAID-gastropathy – nausea, vomiting, heartburn, anorexia, epigastric discomfort or pain, diarrhea, flatulence; rarely – erosive and ulcerative lesions, bleeding; impaired liver function, hepatitis, pancreatitis; irritation or dryness in the oral cavity, mouth pain, ulceration of the gum mucosa, aphthous stomatitis; constipation.

From the nervous system: headache, dizziness, insomnia, anxiety, nervousness, irritability, agitation, drowsiness, depression, confusion, hallucinations; rarely – aseptic meningitis (more often in patients with autoimmune diseases).

From the sensory organs: hearing loss, tinnitus, visual disturbances, toxic optic nerve damage, blurred vision or diplopia, scotoma, amblyopia.

From the cardiovascular system: heart failure, increased blood pressure, tachycardia.

From the hematopoietic organs: anemia (including hemolytic and aplastic), thrombocytopenia, thrombocytopenic purpura, agranulocytosis, leukopenia.

From the respiratory system: shortness of breath, bronchospasm.

From the urinary system: allergic nephritis, acute renal failure, nephrotic syndrome, edema, polyuria, cystitis.

Allergic reactions: skin rash, itching, urticaria, angioedema, bronchospasm, dyspnea, allergic rhinitis, dryness and irritation of the eyes, swelling of the conjunctiva and eyelids, eosinophilia, fever, anaphylactic shock, erythema multiforme exudativum (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Laboratory parameters: decreased serum glucose concentration, decreased hematocrit and hemoglobin, increased bleeding time, increased serum creatinine concentration, increased activity of liver transaminases.

Other: increased sweating.

With long-term use in high doses: ulceration of the gastrointestinal mucosa, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual impairment (impaired color vision, scotoma, amblyopia).

Contraindications

Peptic ulcer of the stomach and duodenum in the acute phase; gastrointestinal bleeding; severe renal failure (creatinine clearance less than 30 ml/min); complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history); optic nerve damage; genetic absence of glucose-6-phosphate dehydrogenase; blood system diseases; period after coronary artery bypass surgery; progressive kidney diseases; severe hepatic failure or active liver disease; confirmed hyperkalemia; inflammatory bowel diseases; children under 2 years of age (for dosage forms containing 100 mg ibuprofen); children and adolescents under 18 years of age (for dosage forms containing more than 200 mg ibuprofen); III trimester of pregnancy, breastfeeding period; hypersensitivity to ibuprofen, paracetamol, to other NSAIDs.

With caution

History of a single episode of gastric ulcer or gastrointestinal ulcer bleeding, gastritis, enteritis, colitis, impaired renal function, liver function, arterial hypertension and/or heart failure, cerebrovascular diseases, diabetes mellitus, blood diseases of unknown etiology (leukopenia, anemia, thrombocytopenia), I and II trimesters of pregnancy, elderly age.

In children over 2 years of age, preparations containing the combination ibuprofen + Paracetamol are used in dosage forms intended for the corresponding age category.

Use in Pregnancy and Lactation

In the I and II trimesters of pregnancy, use is possible only as prescribed by a doctor in cases where the potential benefit outweighs the possible risk to the mother and the potential risk to the fetus. The use of this combination in the III trimester of pregnancy is contraindicated.

If it is necessary to use during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Use is contraindicated in children under 2 years of age.

In children over 2 years of age, preparations containing the combination ibuprofen + Paracetamol are used in dosage forms intended for the corresponding age category.

Special Precautions

With caution: coronary artery disease, chronic heart failure, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, creatinine clearance less than 60 ml/min, history of gastrointestinal ulcerative lesions, presence of Helicobacter pylori infection, elderly age, long-term use of NSAIDs, alcoholism, severe somatic diseases, simultaneous use of oral glucocorticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), viral hepatitis, mild or moderate hepatic and/or renal failure, benign hyperbilirubinemias (Gilbert’s syndrome, Dubin-Johnson syndrome, Rotor syndrome), liver cirrhosis with portal hypertension, nephrotic syndrome.

Simultaneous use with other medicinal products containing Paracetamol and/or NSAIDs should be avoided. When using the drug for more than 5-7 days as prescribed by a doctor, peripheral blood counts and liver functional state should be monitored.

When used simultaneously with indirect anticoagulants, indicators of the blood coagulation system should be monitored.

Concomitant use of this combination with other NSAIDs should be avoided.

To avoid possible damaging effects on the liver, alcohol should not be consumed during the period of drug use.

The drug may distort the results of laboratory tests in the quantitative determination of glucose, uric acid in blood serum, 17-ketosteroids (it is necessary to discontinue the drug 48 hours before the study).

Effect on ability to drive vehicles and mechanisms

During the treatment period, the patient should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interactions

With simultaneous use with acetylsalicylic acid, ibuprofen reduces its anti-inflammatory and antiplatelet effect (an increase in the frequency of acute coronary insufficiency development is possible in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen).

Combination with ethanol, glucocorticosteroids increases the risk of erosive and ulcerative lesions of the gastrointestinal tract.

Ibuprofen enhances the effect of direct (heparin) and indirect (coumarin and indandione derivatives) anticoagulants, thrombolytic agents (alteplase, anistreplase, streptokinase, urokinase), antiplatelet agents, colchicine – the risk of hemorrhagic complications increases.

This combination enhances the hypoglycemic effect of insulin and oral hypoglycemic medicinal products.

It weakens the effects of antihypertensive medicinal products and diuretics (by inhibiting the synthesis of renal prostaglandins).

Increases the concentration in the blood of digoxin, lithium preparations and methotrexate.

Caffeine enhances the analgesic effect of ibuprofen.

With simultaneous use of this combination with cyclosporine, gold preparations, nephrotoxicity increases.

With simultaneous use of this combination with cefamandole, cefoperazone, cefotetan, valproic acid, plicamycin, the frequency of hypoprothrombinemia development increases.

Antacids and cholestyramine reduce the absorption of the ibuprofen+Paracetamol combination.

Myelotoxic medicinal products contribute to the manifestation of hematotoxicity of the ibuprofen+Paracetamol combination.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.